Antiestrogens and selective estrogen receptor

Jordan VC. Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions. / Med Chem 2003 46 883-908. 

Antiestrogens and selective estrogen receptor modulators as multifunctional medicines 03JMC883, 03JMC1081. 

Steiner, M.S. and Raghow, S.,Antiestrogens and selective estrogen receptor modulators reduce prostate cancer risk. World J. Urol, 21, 31-36,2003. 

ANTIESTROGENS AND SELECTIVE ESTROGEN RECEPTOR MODULATORS (SERMs) [SEDA-31, 664 SEDA-32, 743 SEDA-33, 859]... 

Idoxifene is another of the newer selective estrogen receptor modulators (SERMs), and preclinical data show that it has greater antiestrogenic activity than tamoxifen but lower estrogenic activity. It is not yet clear whether this affects its degree of usefulness or safety when it is used, for example, in cases of metastatic breast cancer. In comparisons of the two drugs in such patients the desired effects were similar and the incidence of adverse effects was essentially the same (14). 

Figure 23-16 Selective estrogen receptor modulators (SERMs) and antiestrogens.

Antiestrogen approaches for the therapy of hormone-receptor positive breast cancer include the use of selective estrogen-receptor modulators (SERMs), selective estrogen receptor downregulators (SERDs), and aromatase inhibitors (AIs). 

SELECTIVE ESTROGEN RECEPTOR MODULATORS AND ANTIESTROGENS SERMs TAMOXIFEN, RALOXIFENE, AND TOREMIFENE Selective ER modulators, or SERMs, exert tissue-selective actions. Their pharmacological goal is to produce beneficial estrogenic actions in certain tissues (e.g., bone, brain, and Uver) but antagonist activity in others... 

Tamoxifen citrate, which is classified chemically as a triarylethylene, was developed as an antiestrogenic drug and as a selective estrogen receptor modulator (SERM). It is prescribed for the treatment of metastatic breast cancer. Raloxifene hydrochloride, a benzothiophene... 

The clinical significance of the selective estrogen receptor modulators (SERMs) is well documented. The intensive research is currently directed at discovery of the ideal SERM , an agent that is antiestrogenic in breast and endometrial tissue, but pro-estrogenic in the vasculature and brain, which would be of use as a preventative in breast and uterine cancer and an alternate attractive HRT. Compound 1-(R) is a backup development candidate of the bisbenzopyran lead compound in our SERM program. This compound has shown promising preclinical profile with excellent pharmacokinetic properties. The identification and profiles of this novel SERM will be discussed. 

---